EA202090917A1 - OBTAINING PSILOCYBIN, DIFFERENT POLYMORPHOUS FORMS, INTERMEDIATE COMPOUNDS, COMPOSITIONS AND THEIR APPLICATION - Google Patents

OBTAINING PSILOCYBIN, DIFFERENT POLYMORPHOUS FORMS, INTERMEDIATE COMPOUNDS, COMPOSITIONS AND THEIR APPLICATION

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Publication number
EA202090917A1
EA202090917A1 EA202090917A EA202090917A EA202090917A1 EA 202090917 A1 EA202090917 A1 EA 202090917A1 EA 202090917 A EA202090917 A EA 202090917A EA 202090917 A EA202090917 A EA 202090917A EA 202090917 A1 EA202090917 A1 EA 202090917A1
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EA
Eurasian Patent Office
Prior art keywords
psilocybin
compositions
obtaining
application
intermediate compounds
Prior art date
Application number
EA202090917A
Other languages
Russian (ru)
Inventor
Дерек Джон Лондебро
Кристофер Браун
Джилиан Скотт Нортен
Джиллиан Мур
Хемант Патил
Дэвид Николс
Original Assignee
Компасс Патфайндер Лимитед
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First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=60326674&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=EA202090917(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Компасс Патфайндер Лимитед filed Critical Компасс Патфайндер Лимитед
Publication of EA202090917A1 publication Critical patent/EA202090917A1/en

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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/66—Phosphorus compounds
    • A61K31/675—Phosphorus compounds having nitrogen as a ring hetero atom, e.g. pyridoxal phosphate
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02—Phosphorus compounds
    • C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/553—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having one nitrogen atom as the only ring hetero atom
    • C07F9/572—Five-membered rings
    • C07F9/5728—Five-membered rings condensed with carbocyclic rings or carbocyclic ring systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/66—Phosphorus compounds
    • A61K31/661—Phosphorus acids or esters thereof not having P—C bonds, e.g. fosfosal, dichlorvos, malathion or mevinphos
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/30—Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
    • A61K47/36—Polysaccharides; Derivatives thereof, e.g. gums, starch, alginate, dextrin, hyaluronic acid, chitosan, inulin, agar or pectin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/30—Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
    • A61K47/36—Polysaccharides; Derivatives thereof, e.g. gums, starch, alginate, dextrin, hyaluronic acid, chitosan, inulin, agar or pectin
    • A61K47/38—Cellulose; Derivatives thereof
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0053—Mouth and digestive tract, i.e. intraoral and peroral administration
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
    • A61K9/16—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
    • A61K9/1605—Excipients; Inactive ingredients
    • A61K9/1629—Organic macromolecular compounds
    • A61K9/1652—Polysaccharides, e.g. alginate, cellulose derivatives; Cyclodextrin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/2004—Excipients; Inactive ingredients
    • A61K9/2022—Organic macromolecular compounds
    • A61K9/205—Polysaccharides, e.g. alginate, gums; Cyclodextrin
    • A61K9/2054—Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/24—Antidepressants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B63/00—Purification; Separation; Stabilisation; Use of additives
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/04—Indoles; Hydrogenated indoles
    • C07D209/10—Indoles; Hydrogenated indoles with substituted hydrocarbon radicals attached to carbon atoms of the hetero ring
    • C07D209/14—Radicals substituted by nitrogen atoms, not forming part of a nitro radical
    • C07D209/16—Tryptamines
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00—Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13—Crystalline forms, e.g. polymorphs

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • Inorganic Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Biochemistry (AREA)
  • Molecular Biology (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Psychiatry (AREA)
  • Nutrition Science (AREA)
  • Physiology (AREA)
  • Pain & Pain Management (AREA)
  • Hospice & Palliative Care (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Medicinal Preparation (AREA)

Abstract

Изобретение относится к крупномасштабному производству псилоцибина для применения в медицине. Более конкретно, оно относится к способу получения высокой чистоты кристаллического псилоцибина, в частности в форме полиморфа A. Оно также относится к способу производства псилоцибина и промежуточных соединений в его производстве и составам, содержащим псилоцибин.The invention relates to the large-scale production of psilocybin for use in medicine. More specifically, it relates to a process for the production of high purity crystalline psilocybin, in particular in the form of polymorph A. It also relates to a process for the production of psilocybin and intermediates in its production and compositions containing psilocybin.

EA202090917A 2017-10-09 2018-10-09 OBTAINING PSILOCYBIN, DIFFERENT POLYMORPHOUS FORMS, INTERMEDIATE COMPOUNDS, COMPOSITIONS AND THEIR APPLICATION EA202090917A1 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
GB1716505.1A GB2571696B (en) 2017-10-09 2017-10-09 Large scale method for the preparation of Psilocybin and formulations of Psilocybin so produced
PCT/IB2018/057811 WO2019073379A1 (en) 2017-10-09 2018-10-09 Preparation of psilocybin, different polymorphic forms, intermediates, formulations and their use
GB1816438.4A GB2576059B (en) 2017-10-09 2018-10-09 A pharmaceutical formulation comprising psilocybin

Publications (1)

Publication Number Publication Date
EA202090917A1 true EA202090917A1 (en) 2021-01-14

Family

ID=60326674

Family Applications (1)

Application Number Title Priority Date Filing Date
EA202090917A EA202090917A1 (en) 2017-10-09 2018-10-09 OBTAINING PSILOCYBIN, DIFFERENT POLYMORPHOUS FORMS, INTERMEDIATE COMPOUNDS, COMPOSITIONS AND THEIR APPLICATION

Country Status (17)

Country Link
US (10) US10519175B2 (en)
EP (1) EP3694835A1 (en)
JP (3) JP2020536960A (en)
KR (1) KR20200085753A (en)
CN (1) CN111491919A (en)
AU (2) AU2018349279B2 (en)
BR (1) BR112020006947A2 (en)
CA (1) CA3078765A1 (en)
CO (1) CO2020005643A2 (en)
DE (1) DE202018006384U1 (en)
EA (1) EA202090917A1 (en)
GB (4) GB2571696B (en)
IL (2) IL273883B1 (en)
MX (1) MX2020003910A (en)
PH (1) PH12020550246A1 (en)
SG (1) SG11202003198RA (en)
WO (1) WO2019073379A1 (en)

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